期刊
PLOS ONE
卷 16, 期 11, 页码 -出版社
PUBLIC LIBRARY SCIENCE
DOI: 10.1371/journal.pone.0259008
关键词
-
资金
- The Sao Paulo Research Foundation, FAPESP [2017/03552-5, 2016/06931-4, 2018/ 11079-0]
- National Council for Scientific and Technological Development, CNPq [305174/2020-7, 304731-20170, 311746/2017-9]
- Coordenacao de Aperfeicoamento de Pessoal de Ni'vel Superior (CAPES), Brazil [001]
Leishmaniasis is a neglected disease affecting 12 million people mainly in developing countries. The synthesized compound 4f showed promising antileishmanial activity, possibly acting through a dual mechanism against L. infantum.
Leishmaniasis is a neglected disease that affects 12 million people living mainly in developing countries. Herein, 24 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antileishmanial activity. Compound 4f, a furoxan derivative, was particularly remarkable in this regard, with EC50 value of 3.6 mu M against L. infantum amastigote forms and CC50 value superior to 500 mu M against murine peritoneal macrophages. In vitro studies suggested that 4f may act by a dual effect, by releasing nitric oxide after biotransformation and by inhibiting cysteine protease CPB (IC50: 4.5 mu M). In vivo studies using an acute model of infection showed that compound 4f at 7.7 mg/Kg reduced similar to 90% of parasite burden in the liver and spleen of L. infantum-infected BALB/c mice. Altogether, these outcomes highlight furoxan 4f as a promising compound for further evaluation as an antileishmanial agent.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据